含均三唑硫醚的槟榔碱衍生物的合成及舒张血管活性  

Synthesis and vascular relaxing activity of new arecoline analogues containing 1,2,4-triazole sulfanylether

作　　者：杨锐生[1] 胡国强[2] 黄文龙[3] 

机构地区：[1]泸州医学院化学教研室,四川泸州646000 [2]河南大学药学院,河南开封475004 [3]中国药科大学新药研究中心,江苏南京210009

出　　处：《化学试剂》2008年第1期8-10,共3页Chemical Reagents

摘　　要：用3-硫醚-4-胺基-1,2,4-三唑作为槟榔碱酯基的生物电子等排体合成5个新型槟榔碱衍生物,其化学结构经元素分析、IR、1HNMR、MS确证。采用离体血管条法研究了目标化合物体外舒张血管活性。结果表明在1.01×10-5mol/L浓度下化合物3a^3e的血管舒张率与槟榔碱相当。Five novel derivatives were synthesized with 3-alkyhhio-4-amino-1,2,4-triazole as bioisosteres of the ester group of arecoline, and their structures were characterized by IR, ^1HNMR, MS spectra and elementary analysis. The in vitro vascular relaxing activity of target compounds was screened. The compounds 3a-3e had similar degree of vasodilatation activities compared to that of arecoline.

关 键 词：槟榔碱衍生物 四氢吡啶 均三唑 合成 舒张血管活性 

分 类 号：O626.26[理学—有机化学]